article thumbnail

Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

ASPET

Panobinostat is a potent pan-HDAC inhibitor that has been tested in multiple studies for the treatment of brain tumors. There have been contrasting views surrounding its efficacy for the treatment of tumors in the CNS following systemic administration when examined in different models or species.

article thumbnail

Targeted modification of furan?2?carboxaldehydes into Michael acceptor analogs yielded long?acting hemoglobin modulators with dual antisickling activities

Chemical Biology and Drug Design

Aromatic aldehydes, which increase the oxygen affinity of human hemoglobin to prevent polymerization of sickle hemoglobin and inhibit red blood cell (RBC) sickling, have been the subject of keen interest for the development of effective treatment against SCD.

article thumbnail

Pantothenate kinase activation restores brain coenzyme A in a mouse model of pantothenate kinase associated neurodegeneration [Drug Discovery and Translational Medicine]

ASPET

The metabolic stability, protein binding and membrane permeability of BBP-671 all suggest it has the physical properties required to cross the blood brain barrier. BBP-671 treatment elevated brain coenzyme A concentrations, and improved movement and body weight in a PKAN mouse model.

article thumbnail

The Data-Driven Future of Drug Development

DrugBank

For instance, Insilico Medicine , an AI-driven drug discovery company, has leveraged generative models to design novel molecules with desired properties, such as improved solubility and metabolic stability.    Moreover, data science designs novel drugs, such as antibody-drug conjugates (ADC) and bispecific antibodies.

article thumbnail

Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

With 13 preclinical candidates and three AI-designed drugs currently undergoing clinical trials, Insilico is spearheading a revolution in cancer treatment and beyond. Can you provide a summary of the key findings and implications of the preclinical studies on ISM6331 for the treatment of advanced solid tumours?

article thumbnail

Metabolism of macrocyclic drugs

Metabolite Tales Blog

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

Drugs 52
article thumbnail

Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].